Ring Containing Patents (Class 514/559)
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Patent number: 5837728Abstract: Esters and amides of 9-cis-retinoic acid are synthesized, formulated into pharmaceutically acceptable carriers and administered for the treatment of acne vulgaris, cystic acne, hyper-pigmentation, hypo-pigmentation, psoriasis, dermal and epidermal hypoplasia and kerotoses, the reduction of wrinkling of the skin as an incident of aging and actinic damage, normalization of the production of sebum, the reduction of enlarged pores, promoting the rate of wound healing, limiting of scar tissue formation during healing and the like. They are additionally useful for treatment or amelioration of the same additional classes of skin disorders as is retinoic acid itself and other retinoids. These disorders include ichthyoses (e.g., ichthyosis hystrix, epidermolytic hyperkeratosis, and lamellar ichthyosis), follicular disorders (e.g., pseudofolliculites, senile comedones, nevus comidonicas, and trichostatis spinulosa), benign epithelial tumors (e.g.Type: GrantFiled: January 27, 1995Date of Patent: November 17, 1998Assignee: Molecular Design InternationalInventor: William P. Purcell
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Patent number: 5830488Abstract: A quick drying disinfectant composition comprising 50-99 v/v% lower alcohol, a cationic disinfectant and emollient; wherein the composition further comprises cyclic or chain silicone represented by the formula:?(CH.sub.3).sub.2 SiO!.sub.n or HO--?CII.sub.3).sub.2 SiO!.sub.n --IIin which n represents an integer 2-6; and/or ester of polyhydric alcohol and fatty acid having IOB or 0.22-0.85 in which the fatty acid has straight or branched chain. The disinfectant composition of the present invention has sufficient disinfectant effect and quick drying effect without producing skin roughness or stickiness.Type: GrantFiled: September 21, 1994Date of Patent: November 3, 1998Assignee: Shiseido Co., Ltd.Inventors: Takashi Suzuki, Yoshio Asaka
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Patent number: 5821254Abstract: This invention relates to methods and compositions for preventing or treating cancer. Specifically this invention relates to the use of 9-cis-retinoic acid or derivatives thereof in preventing or treating cancers, in particular breast cancer. The invention also relates to compositions of 9-cis-retinoic acid or derivatives thereof and at least one other antineoplastic agent and to the use of such compositions in the prevention or treatment of cancer, in particular breast cancer.Type: GrantFiled: February 17, 1995Date of Patent: October 13, 1998Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Michael B. Sporn, Mario A. Anzano
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Patent number: 5798363Abstract: The present invention relates to the use of tachykinin antagonists, including substance P antagonists and other neurokinin antagonists, in the treatment of emesis. Also described are novel tachykinin antagonists of formula (I), processes for their preparation, pharmaceutical compositions containing them and their medical use. ##STR1## wherein R represents the ring A ##STR2## or 2-pyridinyl or 2-pyridinyl-N-oxide; R.sup.1 is selected from halogen atoms and C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trifluoromethyl, and S(O).sub.n C.sub.1-4 alkyl groups;R.sup.2 and R.sup.3, which may be the same or different, each independently are selected from hydrogen and halogen atoms and C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trifluoromethyl and cyano groups;n represents zero, 1 or 2;and pharmaceutically acceptable salts and solvates thereof.Type: GrantFiled: December 27, 1995Date of Patent: August 25, 1998Assignee: Glaxo Group LimitedInventors: Russell Michael Hagan, Keith Thomas Bunce
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Patent number: 5798388Abstract: A method for treating the disease state in mammals caused by mammalian cells involved in the inflammatory response is disclosed. Mammalian cells participating in the inflammatory response are contacted with an inflammatory response mediator which reduces the undesired inflammatory response and is an antioxidant. The inflammatory response mediator may further provide a cellular energy source and be a building block in the cellular synthesis of other cellular components. Compositions for reducing and treating undesired inflammatory response are also disclosed.Type: GrantFiled: September 6, 1996Date of Patent: August 25, 1998Assignee: Cellular Sciences, Inc.Inventor: Stanley E. Katz
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Patent number: 5792794Abstract: The present invention relates to active derivatives of sphingoid bases. Specifically, the invention relates to retinoylamide based derivatives of sphingoid bases. The present invention describes a method for obtaining these compounds. The invention also relates to the use of these compounds in cosmetic compositions.Type: GrantFiled: April 21, 1997Date of Patent: August 11, 1998Assignee: Gist-Brocades, N.V.Inventors: Johannes W. J. Lambers, Jan Verweij
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Patent number: 5783593Abstract: The present invention provides a compound of the formula ##STR1## which inhibit squalene synthetase and cholesterol biosynthesis and are useful in the treatment of e.g., hyperlipidaemia, atherosclerosis, or fungal infections, processes for the preparation of the compounds of the invention, intermediates useful in these processes, and pharmaceutical compositions containing the compounds.Type: GrantFiled: April 29, 1996Date of Patent: July 21, 1998Assignee: Abbott LaboratoriesInventors: William R. Baker, Saul H. Rosenberg, Anthony K. L. Fung, Todd W. Rockway, Stephen A. Fakhoury, David S. Garvey, B. Gregory Donner, Stephen J. O'Connor, Rajnandan N. Prasad, Wang Shen, David M. Stout, Gerard M. Sullivan
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Patent number: 5780509Abstract: A compound bearing at least two 2,6-diiodophenyl-4-yl groups represented by formula (IV), particularly a polymer composed of two to eight iodinated tyrosine molecules condensed with each other.Type: GrantFiled: January 29, 1997Date of Patent: July 14, 1998Assignee: Muromachi Kagaku Kogyo Kaisha, Ltd.Inventors: Yoshiki Sugihara, Hiroshi Shionoya, Kiyomi Yamatsu
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Patent number: 5776973Abstract: Novel palladium complexes and pharmaceutical compositions comprising the same are provided. Such complexes comprise (palladium).sub.m (lipoic acid).sub.n, wherein m and n are each independently 1 or 2. A process for preparing such complexes is also disclosed. In addition, a method of treatment of tumors and a method of treatment of psoriasis comprising administering the pharmaceutical compositions of the present invention are provided.Type: GrantFiled: October 18, 1995Date of Patent: July 7, 1998Inventor: Merrill Garnett
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Patent number: 5770230Abstract: A stable and lyophilized formulation of prostaglandin E-1 made by the process comprising a) dissolving PGE-1 in a solution of lactose and tertiary butyl alcohol wherein said tertiary butyl alcohol is present in an amount of from about 15% to about 33% volume/volume and the ratio of said lactose to PGE-1 is from about 40,000 to 1 to about 10,000 to 1 weight/weight whereby a formulation of PGE-1 dispersed in lactose is formed; b) adjusting and maintaining the pH of said formulation from about 3.5 to about 6 with an organic acid buffer, c) freezing said formulation to about -50.degree. C.; and d) drying said formulation to obtain a moisture content of less than 1% by dry weight and a tertiary butyl alcohol content of less than 3% by dry weight. Preferably, step c) includes after freezing said formulation to about -50.degree. C., warming to about -25.degree. C. for about 2 hours then refreezing to about -50.degree. C.Type: GrantFiled: December 30, 1996Date of Patent: June 23, 1998Assignee: Pharmacia & Upjohn CompanyInventors: Dirk L. Teagarden, William J. Petre, Paul M. Gold
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Patent number: 5763468Abstract: A quaternary-ammonium-free composition having bactericidal activity for both Gram positive and Gram negative bacteria, and including (i) at least one terpene alcohol and (ii) at least one bactericidal acidic surfactant such as an alkyl polyether carboxylic acid, an alkenyl polyether carboxylic acid, an alkylaryl polyether carboxylic acid or a phosphoric ester of an alkoxylated non-ionic surfactant, particularly a phosphoric mono- or diester, in acidic or partially neutralized form.Type: GrantFiled: September 10, 1996Date of Patent: June 9, 1998Assignee: Action PinInventors: Alain Barranx, Michel Barsacq, Ghislain Dufau, Jean-Paul Lauilhe
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Patent number: 5750496Abstract: A method for controlling infections caused by Cryptosporidium parvum. The method comprises using protease inhibiting compounds, preferably serine protease inhibitors, to inhibit excystation, invasion, and parasite maturation and development. The method is directed to therapeutic treatment of mammals, such as humans, exposed to C. parvum, and additionally as a prophylactic treatment in immunocompromised subjects at high risk for contracting cryptosporidiosis.Type: GrantFiled: August 12, 1996Date of Patent: May 12, 1998Assignee: Utah State UniversityInventors: John R. Forney, Shiguang Yang, Mark C. Healey
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Patent number: 5750515Abstract: The present invention relates to a cancer metastasis inhibitor comprising a benzoic acid derivative as an active ingredient represented by the formula (I) ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are the same or different and each represents hydrogen atom, hydroxyl group or trimethylsilyl group, or R.sub.3 and R.sub.4 are bonded to each other to form a tetramethylene group substituted with lower alkyl group, and X represents group --COCH.dbd.C(OH)--, group --NHCO-- or group --CONH--, provided that when R.sub.3 and R.sub.4 are bonded to each other to form a tetramethylene group substituted with lower alkyl group, X is group --COCH.dbd.C(OH)-- or group --CONH--, use of the benzoic acid derivative for preparing the cancer metastasis inhibitor and method of inhibiting cancer metastasis, characterized in that an effective amount of the benzoic acid derivative is administered to a mammalian animal for inhibiting metastasis of cancer.Type: GrantFiled: November 26, 1996Date of Patent: May 12, 1998Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Jiro Shibata, Konstanty Wierzba, Koji Murakami, Yuji Yamada, Koichi Shudo
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Patent number: 5741523Abstract: A stable and lyophilized formulation of prostaglandin E-1 made by the process comprising a) dissolving PGE-1 in a solution of lactose and tertiary butyl alcohol wherein said tertiary butyl alcohol is present in an amount of from about 15% to about 33% volume/volume and the ratio of said lactose to PGE-1 is from about 40,000 to 1 to about 10,000 to 1 weight/weight whereby a formulation of PGE-1dispersed in lactose is formed; b) adjusting and maintaining the pH of said formulation from about 3.5 to about 6 with an organic acid buffer; c) freezing said formulation to about -50.degree. C.; and d) drying said formulation to obtain a moisture content of less than 1% by dry weight and a tertiary butyl alcohol content of less than 3% by dry weight. Preferably, step c) includes after freezing said formulation to about -50.degree. C., warming to about -25.degree. C. for about 2 hours then refreezing to about 50.degree. C.Type: GrantFiled: March 28, 1996Date of Patent: April 21, 1998Assignee: Pharmacia & Upjohn CompanyInventors: Dirk L. Teagarden, William J. Petre, Paul M. Gold
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Patent number: 5728739Abstract: The differentiation of preadipocytic cells into adipocytic cells, in particular for correcting insulin-resistance disease states in mammalian organisms, notably in humans, for example type II diabetes and cardiovascular disorders such as hypertension and atherosclerosis, is stimulated by treating such preadipocytic cells, or a patient in need of such treatment, with an effective amount of (a) at least one ligand displaying affinity for the nuclear receptors for retinoic acid and/or isomers thereof, preferably at least one ligand displaying a specific affinity for the RAR receptors and even more preferably the RAR-.alpha. receptor and (b) at least one fatty acid, e.g., a polyunsaturated fatty acid.Type: GrantFiled: August 2, 1995Date of Patent: March 17, 1998Assignee: Centre International De Recherches Dermatologiques GaldermaInventors: Gerard Ailhaud, Paul Grimaldi, Irina Safonova, Braham Shroot, Uwe Reichert
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Patent number: 5721275Abstract: Staple, aqueous gel vehicles are provided for the topical application to the skin of irritating active ingredients such as retinoids, particularly tretinoin, with slow release of the active ingredient and minimal irritancy to the skin. The vehicles include a gelling agent effective to form a gel and hold the active ingredient in the aqueous medium for slow release on the skin, and an effective amount of an antioxidant to retard decomposition of the active ingredient. The vehicles and formulations are preferably aqueous emulsions which contain a solubilizing agent for the generally non-water soluble active ingredients, as well as usually an emulsifying agent and/or surfactant. Chelating agents, emollients, preservatives and other adjuvants and additives may also be included in the vehicles and formulations.Type: GrantFiled: January 21, 1992Date of Patent: February 24, 1998Inventor: Gail S. Bazzano
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Patent number: 5718910Abstract: A peroxyacid antimicrobial concentrate and use composition is provided comprising a C.sub.1 to C.sub.4 peroxycarboxylic acid, and a C.sub.6 to C.sub.18 peroxyacid. The combination of these acids produces a synergistic effect, providing a much more potent biocide than can be obtained by using these components separately. Other components can be added to the composition such as hydrotrope coupling agents, stabilizers, etc. An effective antimicrobial use solution is formed at low concentrations when the concentrate composition is diluted with water to a pH in the range of about 2 to 8. Sanitizing of substantially fixed, "in-place" processing lines in dairies, breweries, and other food processing operations is one utility of the composition.Type: GrantFiled: January 13, 1993Date of Patent: February 17, 1998Assignee: Ecolab Inc.Inventors: Thomas R. Oakes, Patricia M. Stanley, Jerome D. Keller
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Patent number: 5718917Abstract: A method for the treatment of erectile dysfunction comprises instilling intra meatally an aqueous solution containing prostaglandin-containing liposomes and a detergent for lysing the liposomes. A pharmaceutical composition for treating erectile dysfunction comprises a two-component system. The first component comprises a predetermined amount of lyophilized prostaglandin-containing liposomes. The second component comprises a predetermined volume of an aqueous solution containing a detergent, preferably PEG(9) octylphenyl ether, for lysing the liposomes. Dissolution of the lyophilized prostaglandin-containing liposomes yields a liquid composition suitable for application to the penis, preferably intra meatally, to effect erection.Type: GrantFiled: December 15, 1995Date of Patent: February 17, 1998Assignee: Harvard Scientific CorporationInventor: Jackie R. See
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Patent number: 5714515Abstract: A pharmaceutical composition comprising as an active phosphorylation poteal enhancing substance and an alpha-keto carboxylic acid or a pharmaceutically-acceptable salt thereof, its use and products containing the same.Type: GrantFiled: May 8, 1996Date of Patent: February 3, 1998Assignee: The United States of America as represented by the Secretary of the ArmyInventor: Rolf Bunger
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Patent number: 5700816Abstract: Combinations of a cyclooxygenase-2 inhibitor and a leukotriene A.sub.4 hydrolase inhibitor are described for treatment of inflammation and inflammation-related disorders.Type: GrantFiled: June 12, 1995Date of Patent: December 23, 1997Inventors: Peter C. Isakson, Gary D. Anderson, Susan A. Gregory
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Patent number: 5698593Abstract: Nodulocystic and conglobate acne in humans can be alleviated by the oral administration of 13-cis-retinoic acid or a derivative thereof. The active ingredient is administered in a dosage of from about 1.5 to about 3 mg/kg of body weight per day for a period of from about two to about four weeks.Type: GrantFiled: April 15, 1993Date of Patent: December 16, 1997Assignee: The United States of America as represented by the Department of Health and Human ServicesInventor: Gary L. Peck
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Patent number: 5696163Abstract: Method of stabilizing polyunsaturates by adding thereto (i) ascorbic acid or an ester or salt thereof, and (ii) a phosphorylated mono- or di-fatty acyl glyceride or a salt thereof, and optionally a tocopherol or tocotrienol antioxidant, and a method of preparing stable pharmaceutical, nutritional or veterinary compositions.Type: GrantFiled: September 12, 1995Date of Patent: December 9, 1997Assignee: Scotia Holdings plcInventors: John B. Cloughley, Bertram J. F. Hudson, Ian Law
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Patent number: 5696104Abstract: The present invention relates to a process for identifying RXR-agonist molecules, characterized in that it comprises the following steps: (i) a sufficient amount of a compound which is an active ligand for at least one receptor of the super-family of steroidal/thyroidal receptors, other than an RXR-receptor-specific ligand, and which can heterodimerize with the RXRs, is applied topically to a part of the skin of a mammal, (ii) a molecule capable of having an RXR-agonist activity is administered systemically or topically to this same mammal, or to this same part of the skin of the mammal, before, during or after step (i), and (iii) the response on that part of the skin of the mammal thus treated is evaluated.Type: GrantFiled: June 19, 1996Date of Patent: December 9, 1997Assignee: Centre International de Recherches Dermatologiques GaldermaInventors: Michel Demarchez, Andre Jomard
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Patent number: 5683724Abstract: The invention is a process for preventing microbial growth in aqueous streams by applying a C.sub.2 -C.sub.12 percarboxylic acid or mixture of such acids to the aqueous stream and to an automated dispensing system for the percarboxylic acids based on a correlation between oxidation-reduction-potential and anti-microbial levels of the aqueous stream. Generally, the process of the invention is applicable to aqueous streams used in any number of applications such as the application of streams for the transport of food products, e.g. fruits or vegetables, into the processing environment and through the various steps of processing.Type: GrantFiled: January 17, 1997Date of Patent: November 4, 1997Assignee: Ecolab Inc.Inventors: Robert D. P. Hei, Timothy A. Gutzmann, Keith D. Lokkesmoe, Scott P. Bennett, Kimberly L. Person Hei
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Patent number: 5681855Abstract: The invention concerns a kit for the preparation of an emulsion containing prostaglandin E.sub.1, a method of preparing the emulsion and a method of preparing the emulsion composition contained in the kit. The emulsion prepared using this kit is suitable for parenteral application.Type: GrantFiled: September 21, 1995Date of Patent: October 28, 1997Assignee: Schwarz Pharma AGInventors: Andreas Schutz, Hans-Jurgen Mika, Frank Sievert
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Patent number: 5674538Abstract: The invention is a process for preventing microbial growth in aqueous streams by applying a C.sub.2 -C.sub.12 percarboxylic acid such as, for example, peracetic, perpropionic, perbutyric, peroctanoic, perglycolic, perlactic, percitric; and the like to the aqueous stream. Generally, the process of the invention is applicable to aqueous streams used in any number of applications such as the application of streams for the transport of food products, e.g. fruits or vegetables, into the processing environment and through the various steps of processing.Type: GrantFiled: March 13, 1995Date of Patent: October 7, 1997Assignee: Ecolab Inc.Inventors: Keith D. Lokkesmoe, Keith E. Olson
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Patent number: 5658942Abstract: Compounds of formula (I): ##STR1## in which: R represents hydrogen, methyl or hydroxy; X represents an alkyl, alkenyl, cycloalkyl, aryl, aralkyl, or heterocyclic group; A represents a single bond, or an alkylene, alkenylene, alkynylene or alkadienylene group; Y represents hydrogen, or an aryl, cycloalkyl or heterocyclic group; have valuable antihypercholesteremic activities and may be used in the treatment of disorders arising from a blood cholesterol imbalance in humans and other animals.Type: GrantFiled: March 7, 1995Date of Patent: August 19, 1997Assignee: Sankyo Company, LimitedInventors: Masaaki Kurabayashi, Hiroshi Kogen, Hiroshi Kadokawa, Hideshi Kurihara, Kazuo Hasegawa, Masao Kuroda
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Patent number: 5654329Abstract: Compounds of the formula ##STR1## where W is (CH.sub.2).sub.n where n is 1 or 2, or n is 0 and W represents lower alkyl groups attached to each oxygen;m is an integer between 1 and 8;R.sub.1 is COOH or a pharmaceutically acceptable salt thereof, COOR.sub.4, CONR.sub.5 R.sub.6, CONR.sub.5 SO.sub.2 R.sub.7, CH.sub.2 OH, CH.sub.2 OR.sub.7, CH.sub.2 O--COR.sub.7, CH.sub.2 O--CONR.sub.5 R.sub.7, CH.sub.2 OCOOR.sub.7, CH.sub.2 NH.sub.2, CH.sub.2 NR.sub.5 R.sub.6, CH.sub.2 NR.sub.5 COR.sub.7, CHO, CH(OR.sub.8).sub.2, CH(OR.sub.9 O), --COR.sub.10, CR.sub.10 (OR.sub.8).sub.2, or CR.sub.10 OR.sub.9 O, where R.sub.4 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R.sub.4 is phenyl or lower alkylphenyl, R.sub.5 and R.sub.6 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or phenyl or lower alkylphenyl, R.sub.7 is alkyl of 1 to 10 carbons, phenyl or lower alkylphenyl, R.sub.8 is lower alkyl, and R.sub.Type: GrantFiled: June 7, 1995Date of Patent: August 5, 1997Assignee: AllerganInventors: Robert M. Burk, David F. Woodward
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Patent number: 5650435Abstract: This invention provides pharmaceutical compositions containing lipoxin compounds and therapeutic uses for the compounds in treating or preventing a disease or condition associated with columnar epithelial inflammation. The invention also discloses methods for screening for compounds useful in preventing columnar epithelial inflammation.Type: GrantFiled: June 29, 1994Date of Patent: July 22, 1997Inventors: James L. Madara, Charles N. Serhan, Sean P. Colgan
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Patent number: 5639773Abstract: This invention relates to an ocular hypotensive agent which comprises a compound represented by the formula: ##STR1## wherein R.sup.1 represents hydrogen or an optionally substituted hydrocarbon residue that may be bound via a hetero atom; R.sup.2 represents hydrogen or a hydrocarbon residue that may have a substituent; R.sup.3 represents a group capable of forming an anion or a group capable of changing thereto; X is a covalent bond between the 2 benzene rings or a spacer having a chain length of 1 to 2 atoms as the linear moiety between the adjoining phenylene group and phenyl group; n represents 1 or 2; ring A is a benzene ring having 1 or 2 optional substituents in addition to the group represented by COOR.sup.2, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 1, 1994Date of Patent: June 17, 1997Assignees: Senju Pharmaceutical Co., Ltd., Takeda Chemical Industries, Ltd.Inventors: Keiji Kubo, Takahiro Ogawa, Takaaki Deguchi
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Patent number: 5614551Abstract: Fatty acid synthase (FAS) is overexpressed by certain infectious organisms that are resistant to most currently available antibiotics. Contrarywise, little FAS expression is identified in patient tissues. Inhibition of fatty acid synthesis is thus selectively toxic to invasive cells, while patient cells with low FAS activity are resistant. This invention provides a method of treating septic patients where fatty acid synthesis by invading cells is inhibited with resultant interruption of the disease process.Type: GrantFiled: January 24, 1994Date of Patent: March 25, 1997Assignee: The Johns Hopkins UniversityInventors: James D. Dick, Francis P. Kuhajda
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Patent number: 5587396Abstract: New topically applied treatments for cellulite are shown by comparative data to effect structural improvements in cellulite-afflicted thigh area tissues including skin-thickening, thigh-firming and thigh-reduction. The disclosed treatments disrupt the skin's water barrier and elevate trans-epidermal water loss (TEWL) for extended periods of weeks or months and include methods of mechanical or solvent action, for example, tape stripping, or acetone washes. Preferred treatments use creams with active ingredients such as lactic acid to elevate TEWL, a retinoid, preferably vitamin A palmitate to disrupt barrier rebuilding and prolong elevation of TEWL levels, and a cerebroside to inhibit lipid synthesis and intensify the TEWL elevation. Diuretics, for immediate esthetic improvements, anti-irritants and anti-oxidants for irritation control are optional ingredients.Type: GrantFiled: August 26, 1994Date of Patent: December 24, 1996Assignee: Mary Kay Inc.Inventor: Walter P. Smith
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Patent number: 5583160Abstract: N-methylated sphingosine used to induce apoptosis.Type: GrantFiled: December 14, 1994Date of Patent: December 10, 1996Assignee: The Biomembrane InstituteInventors: Yasuyuki Igarashi, Sen-Itiroh Hakomori
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Patent number: 5576349Abstract: Disclosed is a method for terminating an existing potentially lethal cardiac arrhythmia, or preventing an imminent potentially lethal cardiac arrhythmia. The method involves administration of all-trans-retinoic acid or an antiarrhythmically active analog. Antiarrhythmic effects of all-trans-retinoic acid occur within minutes.Type: GrantFiled: November 30, 1995Date of Patent: November 19, 1996Assignee: The General Hospital CorporationInventors: Alexander Leaf, Jing X. Kang
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Patent number: 5538982Abstract: The present invention relates to the use of tachykinin antagonists, including substance P antagonists and other neurokinin antagonists, in the treatment of emesis. Also described are novel tachykinin antagonists of formula (I), processes for their preparation, pharmaceutical compositions containing them and their medical use. ##STR1## wherein R represents the ring A ##STR2## or 2-pyridinyl or 2-pyridinyl-N-oxide; R.sup.1 is selected from halogen atoms and C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trifluoromethyl, and S(O).sub.n C.sub.1-4 alkyl groups;R.sup.2 and R.sup.3, which may be the same or different, each independently are selected from hydrogen and halogen atoms and C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trifluoromethyl and cyano groups;n represents zero, 1 or 2;and pharmaceutically acceptable salts and solvates thereof.Type: GrantFiled: June 30, 1994Date of Patent: July 23, 1996Assignee: Glaxo Group LimitedInventors: Russell M. Hagan, Keith T. Bunce
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Patent number: 5536751Abstract: A pharmaceutical composition comprising as an active phophorylation potenl enhancing substance and an alpha-keto carboxylic acid or a pharmaceutically-acceptable salt thereof, its use and products containing the same.Type: GrantFiled: May 9, 1994Date of Patent: July 16, 1996Assignee: The United States of America as represented by the Secretary of the ArmyInventor: Rolf Bunger
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Patent number: 5534261Abstract: Compositions and methods for prevention of adhesion formation, whereby an effective amount of at least one retinoid, e.g., all trans retinoic acid, is administered for a period of time sufficient to permit tissue repair. The retinoid is preferably administered in conjunction with a delivery vehicle (e.g., microcapsules, microspheres, biodegradable polymer films, lipid-based delivery systems such as liposomes and lipid foams, viscous instillates and absorbable mechanical barriers) useful for maintaining local concentrations of the compound at the injury site at an effective level.Type: GrantFiled: January 17, 1995Date of Patent: July 9, 1996Assignee: University of Southern CaliforniaInventors: Kathleen E. Rodgers, Gere S. Dizerega
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Patent number: 5514712Abstract: The present invention relates to the use of oils of chaulmoogra and derivatives thereof, particularly in the form of esters or salts, for preparing a cosmetic or pharmaceutical, particularly dermatological composition, intended for harmonizing the pigmentation of the skin. It concerns in particular a process for harmonizing tanning.Type: GrantFiled: June 14, 1994Date of Patent: May 7, 1996Assignee: Shiseido International FranceInventor: Jacques LeClere
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Patent number: 5508275Abstract: Lipid-selective antioxidants of the formula I(A).sub.a (L)(X).sub.a, (I),in whichA=an antioxidative component,L=a bridging member,X=a lipophilic componenta and a'=independently of one another the numbers 1 or 2.The compounds are used for the protection of lipid-containing substances against oxidation and in pharmaceuticals for the prophylaxis and treatment of diseases in which bioradicals are involved, in particular of coronary, circulatory and vascular diseases.Type: GrantFiled: March 15, 1994Date of Patent: April 16, 1996Assignee: Hoechst AktiengesellschaftInventors: Klaus-Ulrich Weithmann, Gunther Wess, Dirk Seiffge
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Patent number: 5489434Abstract: A peroxyacid antimicrobial concentrate and use composition is provided comprising a C.sub.5 peroxyacid in combination with a C.sub.1 14 C.sub.4 peroxyacid, a C.sub.6 -C.sub.18 peroxyacid, or mixtures thereof. The combination of these peracids produces a synergistic effect, providing a much more potent biocide than can be obtained by using these components separately. Other components can be added to the composition such as hydrotrope coupling agents, stabilizers, etc. An effective antimicrobial use solution is formed at low concentrations when the concentrate composition is diluted with water. Sanitizing of substantially fixed, "in-place" processing lines in dairies, breweries, and other food processing operations is one utility of the composition.Type: GrantFiled: March 13, 1995Date of Patent: February 6, 1996Assignee: Ecolab Inc.Inventors: Thomas R. Oakes, Thomas G. Boufford
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Patent number: 5476852Abstract: A method of topically treating subjects suffering from acne, hyperkeratotic dermatoses and photo-aging of the skin, by administering to the skin of said subjects an effective amount of the antifungal compound ketoconazole and a retinoid is disclosed. Compositions comprising an inert carrier and as active ingredients the compound ketoconazole and a retinoid are described.Type: GrantFiled: August 24, 1993Date of Patent: December 19, 1995Assignee: Janssen Pharmaceutica N.V.Inventor: Gerard F. M. J. Cauwenbergh
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Patent number: 5474782Abstract: A wound-healing composition and method utilizing a compound of the Formula (I) ##STR1## or a pharmaceutically acceptable salt thereof.Type: GrantFiled: May 20, 1994Date of Patent: December 12, 1995Assignee: WoundFast Pharmaceuticals, Inc.Inventors: Rudolph E. K. Winter, Stephen A. Kolodziej, Walter H. Lewis
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Patent number: 5468495Abstract: Striae distensae lesions may be prevented and/or reduced in size by topically applying to the skin affected with the lesions an effective amount of a retinoid, preferably retinoic acid, preferably by daily application in a dermatologically acceptable vehicle, such as a cream base, at a concentration of about 0.025 to 0.1 weight percent retinoic acid. When applied during the striae rubrae stage, the retinoid may be effective to prevent the formation of striae albae lesions, and when applied in either stage, the retinoid may be effective to reduce the width and depth of the lesions, with improved texture and softness.Type: GrantFiled: March 6, 1992Date of Patent: November 21, 1995Inventor: Albert M. Kligman
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Patent number: 5462967Abstract: A feed additive which is effective for preventing and/or treating protozoiasis of livestock such as coccidiosis and for suppressing accumulation of fat of livestock is disclosed, which comprises (a) a triglyceride of a medium-chain fatty acid having 6 to 12 carbon atoms; and (b) at least one substance selected from a medium-chain fatty acid having 6 to 12 carbon atoms, a monoglyceride of the fatty acid and a diglyceride of the fatty acid. A feed for livestock containing the feed additive, and a method for preventing and/or treating protozoiasis of livestock and a method for suppressing excess accumulation of fat of livestock using the feed are also disclosed. The feed and method of the present invention are particularly effective for broiler.Type: GrantFiled: June 16, 1992Date of Patent: October 31, 1995Assignee: Kao CorporationInventor: Masaharu Hayashi
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Patent number: 5462726Abstract: A method is provided for inhibiting or preventing toxicity and other unwanted effects (a) caused by solvents for pharmaceuticals which solvents contain castor oil or ricinoleic acid or derivatives thereof, such as Cremophor, or (b) caused by a drug, such as cyclosporine A, dissolved or suspended in solvents such as ricinoleic acid or castor oil or derivative thereof, employing a thromboxane A.sub.2 receptor antagonist. Solvent compositions containing ricinoleic acid or castor oil or derivatives thereof and a thromboxane A.sub.2 receptor antagonist, and pharmaceutical compositions including a drug, solvent containing ricinoleic acid or castor oil or derivative thereof, and a thromboxane A.sub.2 receptor antagonist are also provided.Type: GrantFiled: December 17, 1993Date of Patent: October 31, 1995Assignee: Bristol-Myers Squibb CompanyInventor: Nicholas J. Lodge
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Patent number: 5459057Abstract: A method and composition for enhancing biological response modifiers, such as promoting cellular differentiation, by using a Vitamin A or an analog thereof and sphingosine or an analog thereof.Type: GrantFiled: January 11, 1993Date of Patent: October 17, 1995Assignee: Emory UniversityInventors: Alfred H. Merrill, Jr., Joseph M. Kinkade, Jr., Victoria L. Stevens
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Patent number: 5439937Abstract: This invention relates to compounds of Formula I and the stereoisomers and pharmaceutically acceptable salts thereof ##STR1## wherein R is alkyl, alkenyl, alkynyl, or cycloalkylalkyl;R.sup.1 is alkyl;R.sup.2 is hydrogen, alkyl;R.sup.6 is alkyl;n is 1 to 5;p is 0 to 6;x is 0 or 2; andR.sup.4 and R.sup.5 are independently hydrogen or alkyl or together with N form a cycloalkylamine.The compounds of Formula I are leukotriene B.sub.4 antagonists and are useful as anti-inflammatory agents and in treating disease conditions mediated by LTB.sub.4.Type: GrantFiled: March 3, 1994Date of Patent: August 8, 1995Assignee: G. D. Searle & Co.Inventors: Stevan W. Djuric, Stephen H. Docter, Stella S. Yu
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Patent number: 5437868Abstract: A peroxyacid antimicrobial concentrate and use composition is provided comprising a C.sub.5 peroxyacid in combination with a C.sub.1 -C.sub.4 peroxyacid, a C.sub.6 -C.sub.18 peroxyacid, or mixtures thereof. The combination of these peracids produces a synergistic effect, providing a much more potent biocide than can be obtained by using these components separately. Other components can be added to the composition such as hydrotrope coupling agents, stabilizers, etc. An effective antimicrobial use solution is formed at low concentrations when the concentrate composition is diluted with water. Sanitizing of substantially fixed, "in-place" processing lines in dairies, breweries, and other food processing operations is one utility of the composition.Type: GrantFiled: April 12, 1993Date of Patent: August 1, 1995Assignee: Ecolab Inc.Inventors: Thomas R. Oakes, Thomas G. Boufford
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Patent number: 5428071Abstract: The compound 9-cis-retinoic acid, its pharmaceutically acceptable salts or its pharmaceutically acceptable esters can be used in the treatment of precancerous or premalignant epithelial lesions as well as in the treatment of malignant tumors of an epithelial nature.Type: GrantFiled: February 24, 1994Date of Patent: June 27, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Werner Bollag, Joseph F. Grippo, Arthur Levin
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Patent number: 5425938Abstract: Cosmetic compositions are described wherein .alpha.-hydroxyacids, .alpha.-ketoacids and related compounds are formed into amine salts through neutralization with a multi-amine functionalized polymer. Particularly preferred are glycolic acid and lactic acid salts of poly(ethylenimine).Type: GrantFiled: January 28, 1994Date of Patent: June 20, 1995Assignee: Chesebrough-Pond's USA Co., Division of Conopco, Inc.Inventors: Alexander P. Znaiden, Anthony W. Johnson, Brian A. Crotty